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"Kanker kolorektal merupakan salah satu jenis kanker dengan tingkat prevalensi tinggi. Terapi saat ini berupa tindak bedah, radioterapi dan kemoterapi masih memiliki kelemahan yaitu kekambuhan, metastasis, resistensi, serta beberapa efek samping, sehingga diperlukan penelitian alternatif pengobatan baru. Asam galat telah dikenal memiliki sifat sitotoksik terhadap berbagai sel kanker meskipun belum optimal. Perubahan struktur asam galat diketahui dapat merubah beberapa sifat fisiko kimia sehingga diharapkan dapet meningkatkan sifat sitotoksiknya terhadap kanker kolorektal. Penelitian ini bertujuan untuk menilai sitotoksisitas asam galat dan beberapa turunan alkil ester dan alkil eter terhadap sel kanker kolorektal HCT-116 secara in vitro. Penelitian dilakukan secara eksperimental dengan memberikan perlakuan kultur sel HCT-116 dengan asam galat dan turunannya dengan varian konsentrasi 1,6mg/mL ppm hingga 51,2 mg/mL. Viabilitas kemudian dihitung dengan mengukur nilai absorbansi yang selanjutnya dianalisis untuk memperoleh nilai IC50. Hasil analisis menunjukkan etil galat, salisil galat, propil galat, dialil-galat, amil galat, isoamil galat, sekunder amil galat, dan trans-2-heksinil-galat memiliki nilai IC50 lebih baik dari asam galat. Hal ini menunjukkan bahwa terdapat perbedaan sitotoksisitas asam galat dibandingkan dengan derivat alkil ester dan alkil eter, dimana modifikasi gugus karboksil secara umum dapat memperbaiki sitotoksisitas derivat asam galat terhadap kultur sel HCT-116 secara pada kondisi in-vitro.

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Colorectal cancer is one of the most prevalent cancer worldwide. Current therapy of colorectal cancer are surgical procedure, radiotherapy, and chemotherapy depends on morbidity of the case. Those therapy still have some limitations such as relapse, metastasis, resistance, and some mild to serious side effects. Gallic acid have been known as cytotoxic agent against various of cancer cells although its effects is not yet optimal. This study aims to measure the in vitro cytotoxicity of alkyl ester derivatives and alkyl eter derivatives compared with gallic acid to colorectal cancer cell HCT 116. This study is an experimental study conducted by treating HCT 116 cells culture with gallic acids and its derivatives at various concentration ranged from 1,6 mg mL to 51,2 mg mL. The viability of cells measured was calculated from absorbance measurement then analyzed to find IC50 values. The results shows etyl gallate, salicyl gallate, propyl gallate, dialyl gallate, amyl gallate, isoamyl gallate, 1 metyl butyl gallate, and trans 2 hexinyl gallate have better IC50 value compared to gallic acid. This results shows that there are difference of cytotoxicity of gallic acid derivatives compared to gallic acid. The modifications of carboxyl groups generally improve cytotoxicity of gallic acids on culture of colorectal cancer cells HCT 116."

"Latar Belakang: Kanker kolorektal merupakan salah satu kanker dengan prevalensi yang cukup tinggi dan penanganan yang tersedia dapat menyebabkan efek samping buruk. Oleh karena itu, pengobatan alternatif untuk kanker kolorektal perlu dikembangkan. Asam galat telah menunjukkan aksi menghambatan proliferasi sel di berbagai tipe sel kanker termasuk HCT 15 colon cancer cells. Penambahan grup hidrofobik ke asam galat diduga dapat meningkatkan efek anti kanker asam galat. Riset ini dilakukan untuk mengobservasi efek antikanker derivat asam galat, (enam senyawa alkil amida galat hasil sintesis) terhadap sel kolon karsinoma HCT 116. Metode: Menggunakan MTT, enam (6) senyawa alkil amida galat, yaitu: -metil, -etil, -butil, -sek-butil, -ters-butil dan heksil amida galat diuji efek antikankernya terhadap sel HCT 116. Penentuan nilai IC50 dilakukan dengan menggunakan metoda regresi linear untuk analisis data. Hasil uji efek antikanker senyawa turunan alkil amida galat dibandingkan dengan hasil uji efek antikanker asam galat sebagai senyawa awal dan doxorubicin sebagai kontrol positif. Jika dibandingkan dengan asam galat (IC50: 0.05 μg/mL) dan doxorubicin (IC50: 0.001 μg/mL), keenam senyawa turunan alkil amida galat memiliki aktivitas antikanker yang lebih rendah terhadap sel kanker kolon HCT 116. Diantara ke-enam senyawa alkil amida galat hasil sintesis, heksil amida galat dengan IC50 0,07 μg/mL memiliki aktivitas antikanker terbaik. Kesimpulan: Dari hasil studi yang telah dilakukan ini, dapat disimpulkan bahwa heksil amida galat memiliki potensi untuk dikembangkan menjadi agen antikanker kolon.

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Background: Colorectal cancer is one of the most prevalent cancers and its common managements still evoke undesirable side effects. Therefore, there needs to be a development of a safer alternative. Gallic acid has exhibited significant cell proliferation inhibition in a variety of cancer cell lines including HCT 15 colon cancer cells. Addition of hydrophobic groups to gallic acid has been postulated to increase the anti-cancer effects of gallic acid and henceforth this research is conducted to observe the derivatives of gallic acid (six derivative compounds of alkyl amide gallate) on HCT 116 cells. Methods: With the utilization of MTT assay, six synthesized compounds of alkyl amide gallate, namely methyl-, ethyl-, butyl-, sec-butyl-, tert-butyl-, and hexyl amide gallate were measured for their anticancer effect on HCT 116 cells. Determination of IC50 values was carried out by the linear regression method for data analysis. Lastly, results were compared with gallic acid as an original compound and doxorubicin as a positive control. Results: In comparison to gallic acid (IC50: 0.05 μg/mL) and doxorubicin (IC50: 0.001 μg/mL), a lower anticancer effect on colon HCT 116 cells was displayed by all the six- synthesized alkyl amide gallates. Hexyl amide gallate with IC50 value of 0.07 μg/mL shows the strongest anticancer and inhibitory effect on HCT 116 cells. Conclusion: Result of the study indicates that hexyl amide gallate has the potential to undergo further development as a promising anti- colon cancer agent."

"Kanker kolorektal merupakan suatu tumor ganas yang menyerang kolon dan menjadi penyebab kematian terbanyak kedua di Indonesia. Sementara, hingga saat ini, belum ada pengobatan yang efektif. Makroalga Gracilaria verrucosa merupakan salah satu spesies yang belum banyak diteliti, tetapi diduga memiliki efek sitotoksik dan antioksidan. Penelitian terhadap Gracilaria verrucosa ini bertujuan untuk mengetahui efek sitotoksik yang dimiliki pada sel line kanker HCT 116. Penelitian dilakukan dengan ekstraksi makroalga menggunakan pelarut etanol, kloroform, etil asetat, dan n-heksana setelah sebelumnya makroalga diuji kandungan metabolit sekundernya melalui uji fitokimia. Kemudian, 20 L dari setiap ekstrak dimasukkan ke sel HCT 116 yang sebelumnya sudah dicampurkan 100 L DMEM dan diinkubasi selama 24 jam. Setiap sampel kemudian diencerkan secara triplo dalam 8 konsentrasi yaitu 1,5625 g/ml; 3,125 g/ml; 6,25 g/ml; 12,5 g/ml; 25 g/ml; 50 g/ml; 100 g/ml; dan 200 g/ml. Selanjutnya, setiap sampel yang sudah diinkubasi selama 24 jam diujikan aktivitas antikankernya sebagai penghambat pertumbuhan sel kanker kolorektal HCT-116 menggunakan metode MTT assay pada panjang gelombang 490 nm. Data yang diperoleh kemudian dianalisis untuk menghasilkan nilai IC50. Hasil penelitian menunjukkan bahwa keempat ekstrak menunjukkan penghambatan terhadap pertumbuhan sel kanker HCT-116 dengan nilai IC50.

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Colorectal cancer is one of malignant tumors that occurs in colon area. This cancer has become the second killer in Indonesia, after lung cancer. Up until now, there is no effective cure. Macroalgae Gracilaria verrucosa is one of Gracilaria species which has been identified, but is supposed to have anti cytotoxic and anti oxidant effect. This experiment uses Gracilaria verrucosa to identify the cytotoxic effect towards HCT 116 cancer cell. The experiment has extracted Gracilaria verrucosa into four different solvents alkocol, chloroform, ethyl acetate, and n n heksanae. Before extraction, macroalgae was used for phytochemical test in order to identify the secondary metabolit contained in Gracilaria verrucosa. Aftrer extracton, 20 L of the extract then was put into HCT 116 cells which has been mixed with 1 00 L DMEM and incubated for 24 hours. Every sample, afterwards, mixed as triplo in eight concentrations 1,5625 g ml 3,125 g ml 6,25 g ml 12,5 g ml 25 g ml 50 g ml 100 g ml and 200 g ml. Sample extract which has been incubated for 24 hours then was analyzed using MTT assay with 490nm wavelength to identify the anti cancer activity as inhibitor of colorectal cancer HCT 116 cells. Data collected from the experiment would be analyzed so that the researcher can know IC50 value. The result of experiment shows that all of the extract can be used as growth inhibitor of HCT 116 colorectal cancer cells with IC50 value below 100. Meanwhile, the ethanol extract of Gracilaria verrucosa has been proved as the best growth inhibitor due to its lowest IC50 value. From the data, it has been concluded that Gracilaria verrucosa extract has a potential use as a new anti colorectal ancer agent of HCT 116 cells. Keywords phytochemical analysis, Gracilaria verrucosa, cytotoxic effect, colorectal cancer HCT 116 cells "

"Kanker kolorektal, yang merupakan kanker ketiga tersering di dunia, telah menjadi persoalan di seluruh dunia. Dibutuhkan strategi baru untuk pencegahan dan penyembuhannya. Asam salisilat telah terbukti memiliki efek antikanker terhadap sel kanker kolorektal, sehingga mendorong penelitian lebih lanjut untuk mengetahui efek senyawa turunan asam salisilat terhadap pertumbuhan sel HT-29. Senyawa turunan asam salisilat yang digunakan dalam penelitian ini merupakan metil salisilat, etil salisilat, butil salisilat, isoamil salisilat, dan oktil salisilat. Pertama penulis akan melakukan kromatografi lapis tipis serta dengan mengobservasi sifat fisika dan kimia dari senyawa-senyawa tersebut.. Lalu, analisa dari sifat antikanker kelima senyawa tersebut dilakukan menggunakan uji MTT, aktivitas antikanker dinyatakan dengan persentasi inhibisi dan nilai IC50. Kelima senyawa turunan asam salisilat menunjukkan efek penghambatan terhadap pertumbuhan sel HT-29. Nilai IC50 yang didapatkan adalah sebagai berikut; metil salisilat: 117,941 μg/mL, etil salisilat: 6,657 μg/mL, butil salisilat: 58,851 μg/mL, isoamil salisilat: 187,923 μg/mL, oktil salisilat: 116,545. Etil salisilat merupakan senyawa antikanker aktif, sedangkan butil salisilat tergolong cukup aktif. Tiga senyawa lainnya tergolong antikanker lemah. Tidak ada korelasi antara panjang senyawa dan aktivitas antikanker, walaupun kemungkinan adanya korelasi dengan struktur senyawa

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Colorectal cancer (CRC), the third most common cancer worldwide, has been a major problem throughout the world. Novel strategies are needed to prevent and cure it. As salicylic acid has been proven to have chemopreventive and cytotoxic effect towards colorectal cancer cells, we explore its derivatives effects on HT-29 cells. We use five salicylic acid derivatives, namely methyl salicylate, ethyl salicylate, butyl salicylate, isoamyl salicylate, and octyl salicylate. The success of the synthesis is observed through thin layer chromatography and by observing their physical and chemical properties. Then, we use MTT assay to obtain the five salicylic acid derivatives’ anticancer effect, which are presented through their percentage of inhibition and IC50 value.. All five salicylic acid derivatives exhibit inhibitory effects towards the growth of HT-29 colorectal cancer cells. The IC50 value obtained are as follows; methyl salicylate: 117,941 μg/mL, ethyl salicylate: 6,657 μg/mL, butyl salicylate: 58,851 μg/mL, isoamyl salicylate: 187,923 μg/mL, octyl salicylate: 116,545. Ethyl salicylate is classified as an active anticancer compound, butyl salicylate is a moderately active compound. The rest are weakly active anticancer compounds. There is no correlation between compound length and anticancer activity, although there might be one with compound structure."

"[Asam galat merupakan zat polifenol dengan kemampuan sitotoksik. Studisebelumnya menunjukkan turunan asam galat mampu menghambat pertumbuhansel kanker. Sampai saat ini, belum banyak studi yang mempelajari turunan alkilester galat dan turunan metoksi galat terhadap pertumbuhan kanker kolon. Tujuandari penelitian ini adalah untuk mengetahui aktivitas sitotoksik turunan alkil estergalat dan metoksi galat pada sel kanker kolon. Penelitian ini dilakukan dengandesain eksperimental secara in vitro. Kemampuan sitotoksik asam galat danturunannya diuji pada sel HCT116 (sel kanker kolon) dengan menggunakan MTS(3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2Htetrazolium)assay. Data yang diperoleh dianalisis untuk mendapatkan IC50 setiapsenyawa. Hasil penelitian menunjukkan modifikasi asam galat menjadi senyawametil galat, propil galat, butil galat, t-butil galat, amil galat, oktil galat dan ketigaturunan metoksi galat tidak menunjukkan peningkatan aktivitas sitotoksik denganpeningkatan konsentrasi yang diuji. Dari semua senyawa yang memilikikecenderungan menghambat, heptil galat memiliki aktivitas yang paling baik.Disimpulkan, metil galat, propil galat, butil galat, t-butil galat, amil galat, dan oktilgalat merupakan turunan alkil galat yang tidak aktif. Etil galat, isobutil galat,isoamil galat, dan heptil galat merupakan turunan alkil galat yang memiliki aktivitassitotoksik pada sel kanker kolon. Ketiga tur;Gallic acid is a polyphenol with anticancer activity. Previous studies had shown thatthe derivatives of gallic acid had cytotoxic activity in cancer cell. To date, fewstudies evaluated the activity of alkyl ester derivatives of gallic acid and methoxyderivatives of gallic acid in colon cancer cell. The objective of this study was toexamine the cytotoxic activity of alkyl ester derivatives and methoxy derivatives ofgallic acid in colon cancer cell. This study was conducted in in-vitro study inHCT116 colon cancer cell. Cytotoxic activity of gallic acid and its derivatives wereevaluated in HCT116 colon cancer cell using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Data fromthis experiment was analyzed to obtain IC50 of each compound. The result showedthat modification of gallic acid to methyl gallate, propyl gallate, butyl gallat, t-butylgallate, pentyl gallate, octyl gallate and three methoxy derivatives of gallic acid didnot increase cytotoxic activity in all concentrations tested. Among all derivatives ofgallic acid, heptyl gallate has the best cytotoxic activity. In conclusion, methylgallate, propyl gallate, butyl gallate, t-butyl gallate, pentyl gallate, and octyl gallateare alkyl ester derivatives of gallic acid with no cytotoxic activity. Ethyl gallate,isobutyl gallate, isopentyl gallate, and heptyl gallate are active derivatives of gallicacid. All methoxy derivatives of gallic acid do not show any cytotoxic activity incolon cancer cell.;Gallic acid is a polyphenol with anticancer activity. Previous studies had shown thatthe derivatives of gallic acid had cytotoxic activity in cancer cell. To date, fewstudies evaluated the activity of alkyl ester derivatives of gallic acid and methoxyderivatives of gallic acid in colon cancer cell. The objective of this study was toexamine the cytotoxic activity of alkyl ester derivatives and methoxy derivatives ofgallic acid in colon cancer cell. This study was conducted in in-vitro study inHCT116 colon cancer cell. Cytotoxic activity of gallic acid and its derivatives wereevaluated in HCT116 colon cancer cell using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Data fromthis experiment was analyzed to obtain IC50 of each compound. The result showedthat modification of gallic acid to methyl gallate, propyl gallate, butyl gallat, t-butylgallate, pentyl gallate, octyl gallate and three methoxy derivatives of gallic acid didnot increase cytotoxic activity in all concentrations tested. Among all derivatives ofgallic acid, heptyl gallate has the best cytotoxic activity. In conclusion, methylgallate, propyl gallate, butyl gallate, t-butyl gallate, pentyl gallate, and octyl gallateare alkyl ester derivatives of gallic acid with no cytotoxic activity. Ethyl gallate,isobutyl gallate, isopentyl gallate, and heptyl gallate are active derivatives of gallicacid. All methoxy derivatives of gallic acid do not show any cytotoxic activity incolon cancer cell., Gallic acid is a polyphenol with anticancer activity. Previous studies had shown thatthe derivatives of gallic acid had cytotoxic activity in cancer cell. To date, fewstudies evaluated the activity of alkyl ester derivatives of gallic acid and methoxyderivatives of gallic acid in colon cancer cell. The objective of this study was toexamine the cytotoxic activity of alkyl ester derivatives and methoxy derivatives ofgallic acid in colon cancer cell. This study was conducted in in-vitro study inHCT116 colon cancer cell. Cytotoxic activity of gallic acid and its derivatives wereevaluated in HCT116 colon cancer cell using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Data fromthis experiment was analyzed to obtain IC50 of each compound. The result showedthat modification of gallic acid to methyl gallate, propyl gallate, butyl gallat, t-butylgallate, pentyl gallate, octyl gallate and three methoxy derivatives of gallic acid didnot increase cytotoxic activity in all concentrations tested. Among all derivatives ofgallic acid, heptyl gallate has the best cytotoxic activity. In conclusion, methylgallate, propyl gallate, butyl gallate, t-butyl gallate, pentyl gallate, and octyl gallateare alkyl ester derivatives of gallic acid with no cytotoxic activity. Ethyl gallate,isobutyl gallate, isopentyl gallate, and heptyl gallate are active derivatives of gallicacid. All methoxy derivatives of gallic acid do not show any cytotoxic activity incolon cancer cell.]"

"Asam galat adalah salah satu senyawa yang berpotensi menjadi obat baru bagi kanker. Banyak penelitian yang telah menguji aktivitas asam galat sebagai antikanker, tetapi asam galat bersifat sangat hidrofilik sehingga sulit untuk menembus membran sel. Untuk meningkatkan aktivitas sitotoksisitas dan hidrofobisitas, dibuat senyawa turunan asam galat yaitu alkil galat dan metoksi galat. Aktivitas diuji pada sel MCF-7 menggunakan MTS (3-(4,5-dimethylthiazol- 2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay dengan inkubasi selama 48 jam. Aktivitas setiap senyawa ditentukan dengan menggunakan nilai IC50. Dari seluruh senyawa yang diuji, isoamil galat, heptil galat dan oktil galat, merupakan senyawa yang aktif sebagai antikanker MCF-7 dengan nilai IC50 58,11; 25,94 dan 42,34. Berdasarkan ekstrapolasi garis, isobutil galat dan juga dapat menurunkan persentase viabilitas sel, meskipun nilai IC50-nya belum dapat ditentukan dari penelitian ini. Metoksi galat tidak memiliki efek penghambatan pada sel kanker payudara MCF-7. Oleh karena itu, dapat disimpulkan bahwa isobutil, isoamil, heptil dan oktil galat merupakan senyawa turunan asam galat yang memiliki aktivitas sitotoksik sedangkan metoksi galat tidak memiliki aktivitas sitotoksik terhadap MCF-7.

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Gallic acid is a potential chemotherapeutic agent. Many studies have proven the anti cancer activity of gallic acid, including in breast cancer. However, gallic acid is a hydrophilic molecule, which restrict the substance from passing the cell membrane. To increase the potential cytotoxicity and its hydrophobicity, two groups of gallic acid derivatives, alkyl gallates and methoxy gallates, were developed. The activity of these derivatives were tested in MCF-7 cell lines, using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4- sulfophenyl)-2H-tetrazolium) assay, and then incubated for 48 hours. Percentage of cell viability over control were assessed. Cytotoxic activities of gallic acid and its derivatives were determined using IC50 values. Among all of the gallic acid derivatives, isoamyl gallate, heptyl gallate and octyl gallate were the most potential drugs to treat MCF-7 breast cancer with IC50 values of 58,11; 25,94 and 42,34 μg/ml, respectively. Based on the trendline prediction, isobutyl gallate also showed cytotoxic activity towards MCF-7, although the IC50 values cannot be determined in this research. Methoxy gallates do not have any inhibitory activity towards breast cancer MCF-7. In conclusion, isobutyl, isoamyl, heptyl and octyl gallate are gallic acid derivatives with cytotoxic activity, while methoxy gallates do not have any cytotoxic activity towards MCF-7."

"Pendahuluan: Asam galat adalah salah satu senyawa aktif yang dapat menyebabkan apoptosis pada sel kanker paru manusia. Aktivitas antikanker paru yang mengesankan dari asam galat mendorong dilakukannya penelitian untuk menguji aktivitas sitotoksik senyawa turunan asam galat (alkil amida galat) terhadap sel kanker paru A549. Metode: Enam senyawa alkil amida galat hasil sintesis, yaitu Senyawa metil amida galat, etil amida galat, butil amida galat, sek-butil amida galat, ters-butil amida galat, dan heksil amida galat diuji aktivitas sitotoksiknya terhadap sel kanker paru A549 dengan metode MTT Proliferation assay. Data yang dihasilkan dianalisa menggunakan analisis regresi linear untuk mendapatkan nilai IC50. Hasil uji aktivitas sitotoksik senyawa alkil amida galat hasil sintesis dibandingkan dengan hasil uji aktivitas sitotoksik asam galat sebagai senyawa asli dan doxorubicin selaku kontrol positif. Hasil: Jika dibandingkan dengan asam galat (IC50: 23.2 μM) dan doxorubicin (IC50: 31.1 μM), keenam senyawa alkil amida galat, yaitu metil amida galat, etil amida galat, butil amida galat, sek-butil amida galat, ters-butil amida galat, dan heksil amida galat memperlihatkan sitotoksisitas yang lebih kuat terhadap sel kanker paru A549 dengan nilai IC50 berkisar dari 5.4 μM hingga 30.0 μM. Kesimpulan: Enam senyawa alkil amida galat berpotensi dikembangkan lebih lanjut sebagai agen antikanker paru.

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Objective: Gallic acid has shown its potential to induce apoptosis in lung cancer cells. Its impressive anti-lung cancer agent prompted us to conduct research that is aimed to evaluate six alkyl amide derivatives of gallic acid against lung cancer A549 cells.

Methods: six synthesized compounds of alkyl amide gallate, which are methyl amide gallate, ethyl amide gallate, butyl amide gallate, sec-butyl gallate, ters-butyl gallate and hexyl amide gallate, will be evaluated their cytotoxicities agains lung A549 cells by MTT Proliferation assay. Linear regression analysis is used to analyzed the data to generate IC50 value. Cytotoxicity results of alkyl amide gallates will be compared with cytotoxicity result of gallic acid as an original compound and with doxorubicin as positive control.

Results: Compared with gallic acid (IC50 23.2 μM) and doxorubicin (IC50 31.1 μM), six derivatives of aklyl amide gallates (methyl-, butyl-, sec-butyl-, ters- butyl, and hexyl amide gallate) shows better cytotoxic activity against lung A549 cells, with IC50 value range from 5.4 μM to 30.0 μM.

Conclusion: Six compounds of Alkyl amide gallate could be further developed as anti-lung cancer agent."

"Prevalensi kanker payudara pada tahun 2020 menduduki peringkat pertama di dunia maupun di Indonesia. Pencarian obat antikanker menggunakan metode komputasi dinilai lebih efektif dan selektif. Asam galat dan turunannya (ester dan amida) merupakan senyawa yang memiliki aktivitas biologis seperti antikanker. Tujuan dari studi ini adalah melakukan analisis secara in-siliko dan in-vitro terhadap senyawa turunan asam galat (N-Alkil galamida) sebagai agen apoptosis sel kanker payudara MCF7. Sebelas senyawa N-Alkil galamida yang telah disintesis dilakukan studi in-siliko meliputi, interaksi protein-protein, interaksi obat-protein, analisis ADMET dan pemodelan molekuler. Tiga senyawa terbaik berdasarkan studi in-siliko diuji aktivitas sitotoksisitasnya pada sel MCF7 menggunakan metode MTT dan analisis apoptosis menggunakan annexin V-FITC/PI dengan flow cytometry. Protein target terpilih, yaitu JUN, AKT1, CASP3 dan CASP7. Senyawa N-Oktil galamida, N-Ters-Butil galamida dan N-Isoamil galamida merupakan tiga senyawa terbaik. Senyawa asam galat dan turunannya, secara analisis prediksi ADMET termasuk dalam kategori aman sebagai kandidat obat. Aktivitas sitotoksik ketiga senyawa tersebut dinyatakan dengan nilai IC50 berturut-turut adalah 205.2 ± 0,44 μM, 372.6 ± 4,09 μM, dan 441.7 ± 1,41 μM. Aktivitas apoptosis mencapai 55 hingga 56% dibandingkan dengan kontrol sel. Senyawa N-Oktil galamida, N-Ters-Butil galamida dan N-Isoamil galamida berpotensi sebagai agen apoptosis pada sel kanker payudara MCF7.

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The prevalence of breast cancer in 2020 is ranked first in the world and in Indonesia. Searching for anticancer drugs using computational methods is considered more effective and selective. Gallic acid and its derivatives (esters and amides) are compounds that have biological activities such as anticancer. In this study, N-Alkyl gallamides were analyzed in-vitro and in-silico for their potential to act as apoptotic agents for MCF7 breast cancer cells. In-silico investigations on eleven N-alkyl gallamide compounds, including protein-protein interactions, drug-protein interactions, ADMET analysis, and molecular modelling, have been conducted. The three best compounds based on in-silico studies were tested for cytotoxicity activity on MCF7 cells using the MTT assay and apoptosis analysis using annexin V-FITC/PI with flow cytometry. Selected target proteins, namely JUN, AKT1, CASP3 and CASP7. According to ADMET study, gallic acid and their derivatives are safe as therapeutic candidates. The cytotoxic activities of the three compounds were expressed by IC50 values of 205.2 ± 0.44 μM, 372.6 ± 4.09 μM, and 441.7 ± 1.41 μM, respectively. Apoptotic activity reached 55 to 56% compared to control cells. The N-Octyl gallamide, N-Ters-Butyl gallamide and N-Isoamil gallamide compounds have the potential as apoptotic agents in MCF7 cells."

"Asam galat merupakan senyawa polihidroksilfenolik yang mempunyai peran penting dalam berbagai aktivitas selektif terhadap banyak sel line. Desain senyawa dengan modifikasi struktur dan mekanisme aksi dari lead compound asam galat diharapkan dapat meningkatkan aktivitas baik lipofilisitas maupun aksi sitotoksiknya. Penelitian ini bertujuan untuk mendesain dan memodifikasi struktur asam galat, melakukan simulasi docking, mensintesis, serta melakukan uji aktivitas sitotoksik senyawa derivat asam galat terhadap sel line kanker kolon HCT-116. Simulasi docking dilakukan dengan beberapa software adalah is MarvinSketch 15.5.11, Chimera 1.10.2, Autodock 4.2, Pymol 1.7.4.5 dan LigPlot v.1.4.5.; sintesis senyawa derivat asam galat melibatkan beberapa reaksi yaitu esterifikasi, metilasi dan hidrolisis; serta melakukan uji sitotoksik terhadap sel kanker kolon HCT-116. Hasil simulasi docking menghasilkan empat senyawa derivat asam galat dengan nilai binding energy terkecil yaitu benzil galat -7,36 kkal/mol , 2-hidroksi benzil galat -7,63 kkal/mol , 4-metoksi- 2-hidroksi benzil galat -7,18 kkal/mol dan feniletil galat -7,47 kkal/mol . Selanjutnya senyawa derivat asam galat disintesis dan dikarakterisasi menggunakan FT-IR, spektrometer Massa, 1H NMR dan 13C NMR. Sintesis senyawa derivat asam galat menghasilkan rendemen masing-masing adalah 62,11 ; 53,25 ; 51,05 dan 58,87 . Uji sitotoksik keempat senyawa derivat asam galat memiliki aktivitas penghambatan yang baik terhadap sel line kanker kolon HCT-116 dengan nilai IC50 masing-masing adalah 24,79 g/mL; 21,82 g/mL; 26,98 g/mL; dan 19,93 g/mL. Senyawa terbaik yang memberikan aktivitas penghambatan terhadap sel kanker kolon HCT-116 adalah feniletil galat dengan IC50 sebesar 19,93 g/mL.

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Gallic acid is a polyhydroxyphenolic compound that has an important role in a variety of selective activity against many cell line. Design modifications of compounds with structures and mechanisms of action of lead compound gallic acid is expected to increase the activity of both lipophilicity and cytotoxic action. This research aims to design and modify the structure of gallic acid, docking simulation, synthesis, and test the cytotoxic activity of gallic acid derivative compounds against colon cancer cell line HCT 116. Docking simulation perfomed with some software is MarvinSketch 15.5.11, Chimera 1.10.2, Autodock 4.2, Pymol 1.7.4.5 and LigPlot v.1.4.5. Synthesis of compound gallic acid derivatives which involves several reaction that is esterification, methylation and hydrolysis. As well as to test the cytotoxic against colon cancer cell HCT 116. Docking simulation results produced four compounds gallic acid derivatives with a value of binding energy smallest that is benzyl gallate 7.36 kcal mol , 2 hydroxy benzyl gallate 7.63 kcal mol , 4 metoksi 2 hydroxy , benzyl gallate 7.18 kcal mol and phenylethyl gallate 7.47 kcal mol . Further synthesized compound gallic acid derivatives with yield respectively is 62.11 53.25 51.05 and 58.87 . Analysis of compound characterization using FT IR, mass spectrometry, 1H NMR and 13C NMR. Test fourth cytotoxic compound gallic acid derivatives have good inhibitory activity against colon cancer cell line HCT 116 with a value IC50 respectively is 24.79 g mL 21.82 g mL 26.98 g mL and 19.93 g L. Compounds that give the best inhibitory activity against colon cancer cells HCT 116 is phenylethyl gallate with IC50 of 19.93 g mL."

"Kanker serviks merupakan kanker dengan prevalensi tertinggi di Indonesia. Tatalaksana kanker serviks saat ini meliputi kemoterapi, radioterapi, dan pembedahan yang relatif mahal dan menimbulkan efek samping. Asam galat adalah senyawa alami yang berpotensi menjadi pengobatan alternatif kanker serviks. Penelitian ini bertujuan untuk mengetahui aktivitas penghambatan asam galat dan derivatnya pada pertumbuhan kultur sel HeLa, yang dinyatakan dengan nilai IC50. Asam galat dan derivatnya dilarutkan dalam phosphate buffered saline PBS , dibuat triplo dengan 8 variasi konsentrasi dalam rentang 0,067-8,533 g/mL. Kultur sel HeLa diencerkan dan ditambahkan 10 mL PBS serta 1 mL dulbecco 39;s modified eagle medium. Viabilitas sel diuji dengan MTT assay. Hasil yang diperoleh menunjukkan terdapat 9 senyawa derivat yang lebih poten sebagai antikanker serviks HeLa dibandingkan asam galat IC50: 3,606 g/mL , yaitu: propil galat IC50: 0,0000674 g/mL , trans-2-heksenil galat IC50: 0,09583 g/mL , cis-2-heksenil galat IC50: 0,19 g/mL , 2-hidroksi-benzil galat IC50: 0,40 g/mL , amil galat IC50: 0,62 g/mL , sekunder-amil galat IC50: 0,73 g/mL , asam 4-cis-2-heksenil-oksi galat IC50: 1,31 g/mL , asam-4-trans-2-heksenil-oksi galat IC50: 1,69 g/mL , dan benzil galat IC50: 2,98 g/mL . Secara umum, hasil penelitian menunjukkan bahwa penambahan rantai alkil ester pada asam galat dapat meningkatkan sitotoksisitasnya terhadap sel HeLa.

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Cervical cancer is a cancer with the highest prevalence in Indonesia. Currently, the treatments of cervical cancer chemotherapy, radiotherapy, and surgery still have side effects and limitations. Gallic acid is a natural compound that could be developed as alternative treatment of cervical cancer. This study aims to determine anticancer activity of gallic acid and its derivatives on the growth of HeLa cell cultures measured by IC50 value. Gallic acid and its derivatives dissolved in phosphate buffered saline PBS , and made into 8 concentrations 0.067 to 8.533 g mL . HeLa cells culture is diluted and added by 10 mL PBS and 1 mL dulbecco 39 s modified eagle medium. HeLa cells viability was tested by MTT assay. Results showed 9 gallic acid derivatives that have greater anticancer activity than gallic acid IC50 3,606 g mL , i.e. propyl gallate IC50 0,0000674 g mL , cis 2 hexenyl gallate IC50 0,19 g mL , 2 hydroxy benzyl gallate IC50 0,40 g mL , amyl gallate IC50 0,62 g mL , sec amyl gallate IC50 0,73 g mL , 4 cis 2 hexenyl oxy gallic acid IC50 1,31 g mL , 4 trans 2 hexenyl oxy gallic acid IC50 1,69 g mL , trans 2 hexenyl gallate IC50 2,79 g mL , and benzyl gallate IC50 2,98 g mL . In general, the results indicate that addition of alkyl ester chain on gallic acid can increase its cytotoxicity against HeLa cells. "